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Home - Products - GPCR/G Protein - Glucagon Receptor - GRA Ex-25

GRA Ex-25

CAS No. 307983-31-9

GRA Ex-25( GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25 )

Catalog No. M13984 CAS No. 307983-31-9

A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 73 In Stock
5MG 128 In Stock
10MG 194 In Stock
25MG 397 In Stock
50MG 584 In Stock
100MG 833 In Stock
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Biological Information

  • Product Name
    GRA Ex-25
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors.
  • Description
    A potent glucagon receptor inhibitor with IC50 of 56 and 55 nM for rat and human glucagon receptors; binds to human glucagon receptor with Ki of 63 nM, moderately inhibits glucagon induced adenylate cyclase (Ki=254 nM); significantly reduces blood glucose caused by exogenous administration of glucagon in rat model (3 mg/kg, i.v.).Diabetes Preclinical.
  • In Vitro
    GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions. GRA Ex-25 has similar affinity to the rat and human glucagon receptors (IC50=56 and 55 nM, respectively).
  • In Vivo
    GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output.
  • Synonyms
    GRA Ex-25 | GRA Ex 25 | GRA Ex25 | GRAEx-25
  • Pathway
    GPCR/G Protein
  • Target
    Glucagon Receptor
  • Recptor
    humanglucagonreceptor|ratglucagonreceptor
  • Research Area
    Metabolic Disease
  • Indication
    Diabetes

Chemical Information

  • CAS Number
    307983-31-9
  • Formula Weight
    563.6085
  • Molecular Formula
    C29H36F3N3O5
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 32 mg/mL
  • SMILES
    C[C@](C1CC[C@H](N(C(NC2C=CC(OC(F)(F)F)=CC=2)=O)CC2C=CC(C(NCCC(O)=O)=O)=CC=2)CC1)(C)C
  • Chemical Name
    β-Alanine, N-[4-[[[trans-4-(1,1-dimethylethyl)cyclohexyl][[[4-(trifluoromethoxy)phenyl]amino]carbonyl]amino]methyl]benzoyl]-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Kurukulasuriya R, et al. Bioorg Med Chem Lett. 2004 May 3;14(9):2047-50. 2. Lau J, et al. J Med Chem. 2007 Jan 11;50(1):113-28.
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